1. Epigenetics
  2. Histone Methyltransferase
  3. BRD4770

BRD4770 

Cat. No.: HY-16705 Purity: 99.77%
Handling Instructions

BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.

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BRD4770 Chemical Structure

BRD4770 Chemical Structure

CAS No. : 1374601-40-7

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10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
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500 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence[1].

IC50 & Target

Histone methyltransferase G9a[1]

In Vitro

BRD4770 (0-20 µM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h[1].
BRD4770 (2.5-5 µM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells[1].
BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected[1].
BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases[1].

Cell Viability Assay[1]

Cell Line: PANC-1 cells
Concentration: 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 20 µM
Incubation Time: 72 hours
Result: Reduced the number of cells after 72 h.

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 2.5 µM, 5 µM
Incubation Time: 24 hours
Result: Decreased H3K9 trimethylation level by 23% in PANC-1 cells.
Molecular Weight

413.47

Formula

C₂₅H₂₃N₃O₃

CAS No.

1374601-40-7

SMILES

O=C(C1=CC=C2C(N=C(NC(C3=CC=CC=C3)=O)N2CCCC4=CC=CC=C4)=C1)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (13.45 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.77%

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Keywords:

BRD4770BRD 4770BRD-4770Histone MethyltransferaseG9aATMATRchromatinmethylationEHMT2H3K9senescentcell-permeableanti-proliferationInhibitorinhibitorinhibit

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BRD4770
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HY-16705
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